1-O-Acetyl-2-amino-2-deoxy-D-mannopyranose | 696580-33-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-O-Acetyl-2-amino-2-deoxy-D-mannopyranose
• 英文别名: [(3S,4R,5S,6R)-3-amino-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl] acetate
• CAS: 696580-33-3
• 化学式: C₈H₁₅NO₆
• 分子量: 221.21
• InChiKey: HLWDCJWADYUUOP-ZTVVOAFPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.3
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  122
• 氢给体数：
  4
• 氢受体数：
  7

文献信息

• Biochemically-activated contrast agents for magnetic resonance imaging
  申请人：Melchior Marco

  公开号：US20050232866A1

  公开（公告）日：2005-10-20

  The present invention provides a class of biochemically-activated MRI contrast agents. The agents include a paramagnetic chelate attached via a linker arm to a relaxivity-modulating group. When the relaxivity-modulating group is removed or otherwise interacts with a targeted substance, the agents are activated by various mechanisms. The activation is detectable by an increase or decrease in the relaxivity of the metal chelate. The agents are useful in the detection of biochemical parameters in cells, tissues and subjects. Exemplary biochemical parameters are markers that are associated with disease states.

  本发明提供了一类生化激活的MRI对比剂。这些对比剂包括一个顺磁螯合物，通过连接臂连接到一个调节弛豫度的基团。当调节弛豫度的基团被移除或与靶物质发生相互作用时，这些对比剂通过各种机制被激活。激活可通过金属螯合物的弛豫度增加或减少来检测。这些对比剂在细胞、组织和受试者中检测生化参数方面非常有用。示例生化参数是与疾病状态相关的标志物。
• O-linked glycosylation of peptides
  申请人：DeFrees Shawn

  公开号：US20050250678A1

  公开（公告）日：2005-11-10

  The present invention provides polypeptides that include an O-linked glycosylation site that is not present in the wild-type peptide. The polypeptides of the invention include glycoconjugates in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response.

  本发明提供了包含一个O-连接糖基化位点的多肽，该位点在野生型多肽中不存在。本发明的多肽包括糖基共轭物，其中一种物质，如水溶性聚合物、生物分子的治疗剂量，通过完整的O-连接糖基残基与多肽共价连接。还提供了制备本发明多肽的方法、含有该多肽的制药组合物以及通过给予本发明多肽的量来治疗、改善或预防哺乳动物疾病的方法。
• O-LINKED GLYCOSYLATION OF PEPTIDES
  申请人：DeFrees Shawn

  公开号：US20080242846A1

  公开（公告）日：2008-10-02

  The present invention provides polypeptides that include an O-linked glycosylation site that is not present in the wild-type peptide. The polypeptides of the invention include glycoconjugates in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response.

  本发明提供了包含一个O-连接糖基化位点的多肽，该位点在野生型多肽中不存在。本发明的多肽包括糖共轭物，其中一种物质，如水溶性聚合物、生物分子的治疗剂量通过完整的O-连接糖基残基与多肽共价连接。本发明还提供了制备本发明多肽的方法、含有该多肽的制药组合物以及通过给予本发明多肽的量来治疗、改善或预防哺乳动物疾病的方法。
• O-LINKED GLYCOSYLATION USING N-ACETYLGLUCOSAMINYL TRANSFERASES
  申请人：DeFrees Shawn

  公开号：US20110177029A1

  公开（公告）日：2011-07-21

  The present invention provides covalent conjugates between a polypeptide and a modifying group, such as a water-soluble polymer (e.g., PEG). The amino acid sequence of the polypeptide includes one or more O-linked glycosylation sequence, each being a substrate for a GIcNAc transferase. The modifying group is covalently linked to the polypeptide via a glycosyl-linking group interposed between and covalently linked to both the polypeptide and the modifying group. In one embodiment, a glucosamine linking group is directly attached to an amino acid residue of the O-linked glycosylation sequence. The invention further provides methods of making polypeptide conjugates. The present invention also provides non-naturally occurring polypeptides that include at least one O-linked linked glycosylation sequence of the invention, wherein each glycosylation sequence is a substrate for a GIcNAc transferase. The invention further provides pharmaceutical compositions that include a polypeptide conjugate of the invention.

  本发明提供了一种多肽和修饰基团（例如PEG）之间的共价结合物。多肽的氨基酸序列包括一个或多个O-连接的糖基化序列，每个序列都是GIcNAc转移酶的底物。通过连接在多肽和修饰基团之间并与两者共价连接的糖基连接基团，将修饰基团共价连接到多肽上。在一种实施方式中，葡萄糖胺连接基团直接连接到O-连接的糖基化序列的氨基酸残基上。本发明还提供制备多肽共轭物的方法。本发明还提供了至少包括本发明中的O-连接的糖基化序列之一的非自然多肽，其中每个糖基化序列都是GIcNAc转移酶的底物。本发明还提供包括本发明的多肽共轭物的制药组合物。
• PURIFICATION OF PEPTIDE CONJUGATES BY HYDROPHOBIC INTERACTION CHROMATOGRAPHY
  申请人：DeFrees Shawn

  公开号：US20120016105A1

  公开（公告）日：2012-01-19

  The present invention provides polypeptides that include an O-linked glycosylation site that is not present in the wild-type peptide. The polypeptides of the invention include glycoconjugates in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. Also provided are methods of making a glycoconjugate, methods of isolating a glycoconjugate from a reaction mixture, pharmaceutical compositions containing a glycoconjugate, and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a glycoconjugate sufficient to achieve the desired response.

  本发明提供了包括一个O-连接糖基化位点的多肽，该位点不存在于野生型多肽中。本发明的多肽包括糖基共轭物，其中一种物种，如水溶性聚合物、生物分子的治疗剂通过完整的O-连接糖基残基与多肽共价连接。还提供了制备糖基共轭物的方法、从反应混合物中分离糖基共轭物的方法、含有糖基共轭物的药物组合物以及通过给予足够量的糖基共轭物来治疗、改善或预防哺乳动物疾病的方法，以达到所需的反应。